TGF-β receptors (Transforming growth factor-β receptors) are single pass serine/threonine kinase receptors. Transforming growth factor beta (TGF-beta) is a member of a large family of pleiotropic cytokines that are involved in many biological processes, including growth control, differentiation, migration, cell survival, adhesion, and specification of developmental fate, in both normal and diseased states. TGF-beta superfamily members signal through a receptor complex comprising a type II and type I receptor, both serine/threonine kinases.
The type I receptors, referred to as activin receptor-like kinases (ALK), lie at the epicenter of the signaling cascade as they transduce TGF-beta signals to intracellular regulators of transcription known as Smad proteins. ALKs possess an extracellular binding domain, a transmembrane domain, a GS domain that serves as the site of activation by type II receptors, and a kinase domain that activates downstream signaling molecules. ALKs mediate the effect of TGF-beta superfamily on a variety of cellular processes such as proliferation, differentiation, apoptosis, adhesion and migration, and therefore play important roles in many biological processes. Some ALKs have been implicated in several disorders, including tumorigenesis and immune diseases, suggesting that these receptors can be used as drug targets.
货号 | 产品名 | Cas | 产品描述 |
---|---|---|---|
PL08591 | (22S,23S)-Homobrassinolide | 80483-89-2 | (22S,23S)-Homobrassinolide 是各种植物生物测定系统中诱导植物生长的最活跃的油菜素类固醇之一。(22S,23S)-Homobrassinolide 在大鼠骨骼肌细胞中显示 Akt 依赖性合成代谢活性。具有口服活性。 |
PL11630 | (24S)-MC 976 | 112849-14-6 | (24S)-MC 976是维他命D3衍生物。 |
PL09434 | (R,R)-BD-AcAc 2 | 1208313-97-6 | (R,R)-BD-AcAc 2((R,R)-Ketone Ester) 是一种酮单酯,可作为口服营养酮的来源。小鼠口服 (R,R)-BD-AcAc 2 后可提高血浆 β-羟基丁酸和乙酰乙酸水平、血糖、血液钠离子水平和血肌酐水平。(R,R)-BD-AcAc 2 可在一定程度上预防脓毒症小鼠的肌无力。(R,R)-BD-AcAc 2 具有提高动物机体运动能力和耐力的潜力。(R,R)-BD-AcAc 2 还可用于研究帕金森病或糖尿病。 |
PL11831 | 1-Cyclohexyl-3-dodecyl urea | 402939-18-8 | 1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) 是一种具有高度选择性的可溶性环氧化物水解酶 (sEH) 抑制剂。1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) 可提高血管紧张素 II (Ang II) 高血压中的环氧二十碳三烯酸 (EETs) 水平并降低血压。 |
PL11781 | 10,12-Tricosadiynoic acid | 66990-30-5 | 10,12-Tricosadiynoic acid 是一种高特异性,选择性,高亲和力且具有口服活性的酰基辅酶 A 氧化酶-1 (ACOX1) 抑制剂。10,12-Tricosadiynoic acid 可改善线粒体脂质和 ROS 代谢,可用于高脂饮食或肥胖引起的代谢性疾病的研究。 |
PL11663 | 123C4 | 2034159-30-1 | 123C4 是一种有效、选择性的,竞争性受体酪氨酸激酶 EPHA4 激动剂,Ki 值为 0.65 μM. |
PL11525 | 2',3'-cGAMP sodium | 2',3'-cGAMP sodium (2'-3'-cyclic GMP-AMP sodium) 是一种哺乳动物细胞中的内源性 cGAMP。2',3'-cGAMP sodium 以高亲和力结合 STING,是干扰素-β (IFNβ) 的有效诱导物。2',3'-cGAMP sodium 是在哺乳动物细胞中为响应细胞质中的 DNA 而产生。 | |
PL11828 | 2,2,14,14-Tetramethyl-8-oxopentadecanedioic acid | 413624-71-2 | 2,2,14,14-Tetramethyl-8-oxopentadecanedioic acid 是一种酮类化合物,详细信息请参考专利文献 WO2002030860A2 中的化合物 II-9。2,2,14,14-Tetramethyl-8-oxopentadecanedioic acid 可用于心血管疾病、血脂异常、蛋白异常和糖代谢紊乱的研究。 |
PL11739 | 2-Methylcitric acid trisodium | 117041-96-0 | 2-Methylcitric acid trisodium (Methylcitric acid trisodium) 是 2- 甲基柠檬酸循环的内源性代谢物。2-Methylcitric acid trisodium 在甲基丙二酸血症和丙二酸酸血症中积累并能作为代谢标志物。2-Methylcitric acid trisodium 对谷氨酸支持的线粒体中 ADP 刺激和不耦合呼吸作用有明显的抑制作用。 |
PL11632 | 24, 25-Dihydroxy VD2 | 58050-55-8 | 24, 25-Dihydroxy VD2是维生素D2的羟基化代谢产物,是合成的维生素D类似物。 |
PL11639 | 3,3-Dimethyl-1-butanol | 624-95-3 | 3,3-Dimethyl-1-butanol (DMB) 是一种口服有效的三甲胺 (TMA) 和三甲基胺-N-氧化物 (TMAO) 抑制剂。3,3-Dimethyl-1-butanol 抑制 p65 NF-κB 和 TGF-β1/Smad3 信号通路。3,3-Dimethyl-1-butanol 在心血管疾病 (CVD) 中有潜在应用。 |
PL08590 | 3,4,5-Trihydroxycinnamic acid decyl ester | 1770778-45-4 | 3,4,5-Trihydroxycinnamic acid decyl ester 是一种高效的脂质吸收和积累抑制剂,具有抗肥胖作用。3,4,5-Trihydroxycinnamic acid decyl ester 是一种胰腺脂肪酶 (pancreatic lipase) 抑制剂,其 EC50 大约为 0.9 μM。 |
PL11688 | 3,5-Dihydroxyacetophenone | 51863-60-6 | 3,5-Dihydroxyacetophenone 是一种内源性代谢产物。 |
PL11784 | 3-Hydroxybutyric acid sodium | 150-83-4 | 3-Hydroxybutyric acid sodium (β-Hydroxybutyric acid sodium) 是一种在 I 型糖尿病中升高的代谢物。3-Hydroxybutyric acid sodium 可以调节膜脂的性质。 |
PL08402 | 3β-Ursodeoxycholic acid | 78919-26-3 | 3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) 是胆汁酸。 3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) 通过口服给药显示出良好的耐受性和良好的肠道吸收。3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) 可以被肠和肝酶异构化并产生 UDCA。 |
PL11735 | 4-Methyl-1-phenyl-2-pentanone | 5349-62-2 | 4-Methyl-1-phenyl-2-pentanone 是一种内源性代谢产物。 |
PL08595 | 5'-Phosphoguanylyl-(3',5')-guanosine | 33008-99-0 | 5'-Phosphoguanylyl-(3',5')-guanosine (pGpG) 是通过酶促环鸟苷二磷酸 (c-di-GMP) 降解途径产生的中间分子。5'-Phosphoguanylyl-(3',5')-guanosine 可用于检测核酸的代谢。 |
PL11610 | [Des-His1,Glu9]-Glucagon amide TFA | [Des-His1,Glu9]-Glucagon amide TFA 是一种有效的胰高血糖素受体的肽拮抗剂,pA2 值为 7.2。 [Des-His1,Glu9]-Glucagon amide TFA 在糖尿病的发病机理研究中有用。 | |
PL11863 | A 83-01 sodium | A 83-01 sodium 是一种有效的 TGF-β I 型受体 ALK5,ALK4 和 ALK7 的抑制剂,能够抑制 ALK5,ALK4 和 ALK7 诱导的转录,IC50 值分别为 12 nM,45 nM 和 7.5 nM。 | |
PL11755 | AC-262536 | 870888-46-3 | AC-262536 是一种选择性的非甾体雄激素受体调节剂 (SARM),具有有益的合成代谢作用。AC-262536 对雄激素受体具有强效激动剂活性,亲和力在低纳摩尔范围 (1-10 nM)。 |